PD 168368 - CAS:204066-82-0

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PD 168368

目录号 : KCM12420 CAS No. : 204066-82-0 纯度 : ≥95%

Data Sheet 产品使用指南

PD 168368 is a competitive antagonist of neuromedin B (NMB) receptors (Ks = 15-45 nM for rat and human receptors expressed in various cell lines). It blocks the elevation of intracellular calcium and release of inositol phosphate induced by NMB in cells expressing NMB receptors. PD 168368 is selective for NMB receptors over those for related peptide agonists, including bombesin and gastrin-releasing peptide. It is also an agonist of formyl-peptide receptors (FPRs) at higher concentrations (ECs = 0.57 and 0.24 µM for FPR1 and FPR2, respectively). PD 168368 induces cell cycle arrest and apoptosis in MDA-MB-231 breast cancer cells and blocks neovascularization and cancer cell growth in breast cancer xenograft tumors in mice.

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock
10 mM * 1 mL in DMSO		In-stock

加入购物车大包装询价

Other Forms of Rapamycin:

Bombesin acetate In-stock
PD 168368 In-stock
ICI 216140 In-stock
Litorin In-stock

KKL Med 的所有产品和服务仅用于科学研究，不能被用于人体，兽医，我们也不向个人提供产品和服务。

生物活性

PD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the K_i of 15–45 nM. PD 168368 is neuromedin B receptor (NMBR; IC₅₀=96 nM) / gastrin-releasing peptide receptor (GRPR IC₅₀=3500 nM) antagonist. PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC₅₀s of 0.57, 0.24, and 2.7 nM, respectively.

体外研究

PD 168368 has high activity and stimulates the release of [Ca²⁺] I in human neutrophils, with EC50 values in the nanomolar range.
PD 168368 inhibits the migration and invasion of human breast cancer cell line MDA-MB-231. PD 168368 reduces epithelial mesenchymal transformation (EMT) of breast cancer cells through up regulation of E-cadherin and down regulation of vimentin. PD 168368 (5 μM) inhibits the migration and invasion of breast cancer cells.
PD 168368 (10 μM) inhibits the activation of mTOR/p70S6K/4EBP1 and AKT/GSK-3 β in breast cancer cells.

Cell Viability Assay

Cell Line:	Human breast cancer cell line MDA-MB-231
Concentration:	5 μM
Incubation Time:	24 hours
Result:	Clearly decreased the migratory ability of MDA-MB-231 cells in a Boyden chamber migration assay.

Cell Viability Assay

Cell Line:	MDA-MB-231 cells
Concentration:	10 μM
Incubation Time:	0, 0.5, 1, 2, 4, 8, and 16 hours
Result:	Decreased phosphorylation levels of mTOR, p70S6K, 4EBP1, AKT and GSK-3β in a time-dependent manner.

体内研究

PD 168368 effectively inhibits the metastasis of breast cancer in vivo. PD 168368 (1.2 mg/kg; intraperitoneal injection for 30 days) inhibits the metastasis of breast cancer in mice.

Animal Model:	Female BALB/c-nude mice (age 8-10 weeks) bearing MDA-MB-231 xenograft model
Dosage:	1.2 mg/kg
Administration:	Intraperitoneal injection for 30 days
Result:	No metastatic tumor nodules were observed in lungs of PD 168368-treated mice compared to PEG-injected mice.

分子式

C₃₁H₃₄N₆O₄

分子量

554.64

CAS号

204066-82-0

中文名称

（S） -α-甲基-α-[[[（4-硝基苯基）氨基]羰基]氨基]-N-[[1-（2-吡啶基）环己基]甲基]-1H-吲哚-3-丙酰胺

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 125 mg/mL (225.37 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8030 mL	9.0149 mL	18.0297 mL
5 mM	0.3606 mL	1.8030 mL	3.6059 mL
10 mM	0.1803 mL	0.9015 mL	1.8030 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO → 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.75 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.75 mM，饱和度未知) 的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL ⽟⽶油中，混合均匀。
2.

请依序添加每种溶剂： 10% DMSO → 40% PEG300→ 5% Tween-80 → 45% saline

Solubility: ≥ 1 mg/mL (1.80 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (1.80 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加⼊ 50 μL Tween-80，混合均匀；然后继续加⼊ 450 μL ⽣理盐⽔定容⾄ 1 mL。
3.

请依序添加每种溶剂： 10% DMSO → 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1 mg/mL (1.80 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (1.80 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中，混合均匀。